Tìm theo
Doxylamine
Các tên gọi khác (8 ) :
  • 2-(alpha-(2-(Dimethylamino)ethoxy)-alpha-methylbenzyl)pyridine
  • 2-Dimethylaminoethoxyphenylmethyl-2-picoline
  • Dossilamina
  • Doxilamina
  • Doxilminio
  • Doxylaminum
  • N,N-Dimethyl-2-(1-phenyl-1-(2-pyridinyl)ethoxy)ethanamine
  • Phenyl-2-pyridylmethyl-beta-N,N-dimethylaminoethyl ether
histamine h1 antagonists, antiemetics
Thuốc Gốc
Small Molecule
CAS: 469-21-6
ATC: R06AA09
ĐG : Amend
CTHH: C17H22N2O
PTK: 270.3694
Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in parkinsonism. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H22N2O
Phân tử khối
270.3694
Monoisotopic mass
270.173213336
InChI
InChI=1S/C17H22N2O/c1-17(20-14-13-19(2)3,15-9-5-4-6-10-15)16-11-7-8-12-18-16/h4-12H,13-14H2,1-3H3
InChI Key
InChIKey=HCFDWZZGGLSKEP-UHFFFAOYSA-N
IUPAC Name
dimethyl({2-[1-phenyl-1-(pyridin-2-yl)ethoxy]ethyl})amine
Traditional IUPAC Name
doxylamine
SMILES
CN(C)CCOC(C)(C1=CC=CC=C1)C1=CC=CC=N1
Độ tan chảy
< 25 °C
Độ sôi
139 °C at 5.00E-01 mm Hg
Độ hòa tan
1 g/ml (succinate salt)
logP
2.5
logS
-2.7
pKa (Strongest Basic)
8.87
PSA
25.36 Å2
Refractivity
82.24 m3·mol-1
Polarizability
31.09 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Doxylamine is an antihistamine commonly used as a sleep aid. This drug is also used to relieve symptoms of hay fever (allergic rhinitis), hives (rash or itching), and other allergic reactions. Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power far superior to virtually every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most powerful over-the-counter sedative available in the United States, and more sedating than many prescription hypnotics. In a study, it was found to be superior to even the barbiturate, phenobarbital for use as a sedative. Doxylamine is also a potent anticholinergic.
Cơ Chế Tác Dụng : Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in parkinsonism. [PubChem] Like other antihistamines, doxylamine acts by competitively inhibiting histamine at H1 receptors. It also has substantial sedative and anticholinergic effects.
Dược Động Học :
▧ Absorption :
Readily absorbed via the gastrointestinal tract.
▧ Metabolism :
Hepatic.
▧ Half Life :
10 hours
Độc Tính : Signs of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, swelling of face, lips, tongue, or throat.
Chỉ Định : Used alone as a short-term sleep aid, in combination with other drugs as a night-time cold and allergy relief drug. Also used in combination with Vitamin B6 (pyridoxine) to prevent morning sickness in pregnant women.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Pramlintide May cause additive slowing of GI motility.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Doxylamine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Doxylamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Doxylamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Doxylamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00366
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3162
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506354
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02327
ChemSpider
http://www.chemspider.com/Chemical-Structure.3050.html
PharmGKB
http://www.pharmgkb.org/drug/PA449419
Wikipedia
http://en.wikipedia.org/wiki/Doxylamine
Drugs.com
http://www.drugs.com/cdi/doxylamine.html
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